Table 1. Database for drugs analyzed in this study. Mechanism of action* Drug† NSC No. mean -log GI50 std dev # expts average # lines/expt MAJ.MOA n1 n2 n3 n4 NSC NAME NOTES REFERENCES Mechanism of action* Drug† NSC No. mean -log GI50 std dev # expts average # lines/expt A2 Mitomycin 26980 6.11 0.56 137 42.9 Db Cyanomorpholinodoxorubicin 357704 10.29 0.32 11 46.1 A2 Porfiromycin 56410 5.43 0.61 13 43.2 ALK A7 C1 750 Busulfan "bis-methanesulfonate, no C2, probably C1" Db Hycanthone 142982 5.10 0.20 9 31.1 A6 Carmustine (BCNU) 409962 4.15 0.22 136 42.5 Db Morpholino-adriamycin 354646 7.73 0.32 8 49.0 A6 Chlorozotocin 178248 3.21 0.40 10 45.8 Db N-N-Dibenzyl-daunomycin 268242 4.83 0.47 15 41.6 A6 Clomesone 338947 3.72 0.38 15 43.1 Db Pyrazoloacridine 366140 6.56 0.29 15 43.4 A6 Lomustine (CCNU) 79037 4.35 0.31 56 38.9 ALK A7 C2 762 Mechlorethamine Di 5-6-Dihydro-5-azacytidine 264880 4.63 0.75 16 40.0 A6 Mitozolamide 353451 3.93 0.31 15 43.0 Di alpha-2'-Deoxythioguanosine 71851 3.80 0.38 15 43.3 A6 PCNU 95466 3.68 0.44 15 42.1 ALK A7 C2 3088 Chlorambucil Di Azacytidine 102816 6.11 0.29 15 44.2 A6 Semustine (MeCCNU) 95441 4.37 0.18 15 39.9 ALK A7 C2 6396 Thiotepa Di beta-2'-Deoxythioguanosine 71261 5.94 0.50 15 44.7 A7 Asaley 167780 5.30 0.44 16 38.3 ALK A7 C2 8806 Melphalan Di Thioguanine 752 5.91 0.46 135 43.3 A7 Busulfan 750 3.22 0.36 4 54.8 ALK A7 C2 9706 Triethylenemelamine tris-aziridine Df Aminopterin 132483 6.18 1.39 3 44.3 A7 Carboplatin 241240 3.88 0.27 59 39.8 Df Aminopterin-derivative 134033 6.60 1.23 3 43.0 A7 Chlorambucil 3088 4.22 0.40 130 42.8 ALK A7 C2 25154 Pipobroman bis-bromide Df Aminopterin-derivative 184692 6.67 1.55 3 47.7 A7 Cisplatin 119875 5.38 0.37 127 41.4 ALK A2 C2 Re 26980 Mitomycin Df an-antifol 623017 7.01 1.40 2 39.0 A7 Cyclodisone 348948 4.41 0.26 14 44.1 Df an-antifol 633713 8.17 0.80 2 50.5 A7 Diaminocyclohexyl-Pt-II 271674 5.51 0.50 16 44.0 Df Baker's-soluble-antifolate 139105 6.24 1.47 5 50.6 A7 Dianhydrogalactitol 132313 4.33 0.51 16 40.4 Df Methotrexate 740 6.94 1.28 4 53.2 A7 Diaziridinylbenzoquinone 182986 5.50 0.42 52 39.0 ALK A7 C2 34462 Uracil mustard Df Methotrexate-derivative 174121 8.05 0.87 3 51.0 A7 Fluorodopan 73754 3.46 0.23 10 39.4 Df Trimetrexate 352122 8.58 1.11 4 50.8 A7 Hepsulfam 329680 3.67 0.38 14 43.4 Dr Guanazole 1895 2.23 0.24 15 44.1 A7 Iproplatin 256927 4.45 0.31 16 40.0 ALK A2 C2 Re 56410 Porfiromycin Dr Hydroxyurea 32065 3.14 0.42 55 39.9 A7 Mechlorethamine 762 5.52 0.57 56 39.9 Dr Pyrazoloimidazole 51143 2.59 0.39 15 43.6 A7 Melphalan 8806 4.56 0.38 56 38.2 Ds Aphidicolin-glycinate 303812 5.02 0.78 14 42.4 A7 Piperazine mustard 344007 3.97 0.51 15 42.8 Ds Cyclocytidine 145668 4.73 1.37 17 38.4 A7 Piperazinedione 135758 6.11 0.57 16 41.6 Ds Cytarabine (araC) 63878 4.82 1.49 132 39.7 A7 Pipobroman 25154 4.16 0.28 56 38.8 ALK A7 Cp 73754 Fluorodopan "ClEtFEt mustard, few C2, maybe DPC" Ds Floxuridine (FUdR) 27640 6.39 1.13 4 54.5 A7 Spiromustine 172112 3.82 0.29 12 33.2 ALK A6 C2 Ca 79037 Lomustine (CCNU) Ds Fluorouracil (5FU) 19893 4.63 0.73 1149 53.6 A7 Teroxirone 296934 4.90 0.47 15 43.3 T2 T2 Db In 82151 Daunorubicin Ds Ftorafur 148958 2.67 0.34 4 51.8 A7 Tetraplatin 363812 5.91 0.52 13 43.8 T1 T1 94600 CPT active Ds Thiopurine (6MP) 755 5.31 0.67 134 42.4 A7 Thiotepa 6396 4.09 0.46 131 42.8 ALK A6 C2 Ca 95441 Semustine (MeCCNU) Rs Acivicin 163501 5.50 0.48 16 39.4 A7 Triethylenemelamine 9706 5.20 0.47 136 43.3 ALK A6 C2 95466 PCNU Rs Dichloroallyl-lawsone 126771 4.97 0.50 16 41.9 A7 Uracil mustard 34462 4.56 0.51 56 40.1 ALK A7 C2 102627 Yoshi-864 bis-methanesulfonate Rs DUP785 (brequinar) 368390 5.80 1.07 10 42.5 A7 Yoshi-864 102627 2.90 0.31 15 44.0 Rs L-Alanosine 153353 5.06 0.74 16 39.8 T1 Camptothecin 94600 7.40 0.58 9 38.3 T1 T1 107124 "CPT,10-OH" active Rs N-phosphonoacetyl-L-aspartic-acid 224131 3.35 0.75 15 39.5 T1 "Camptothecin,7-Cl" 249910 7.42 0.83 5 48.8 Rs Pyrazofurin 143095 5.26 1.03 12 43.6 T1 "Camptothecin,9-MeO" 176323 7.10 0.97 4 52.0 TU Colchicine 757 7.26 1.17 7 45.9 T1 "Camptothecin,9-NH2 (RS)" 629971 7.36 0.74 5 51.2 TU Colchicine-derivative 33410 7.58 0.93 7 47.3 T1 "Camptothecin,9-NH2 (S)" 603071 7.43 0.66 6 49.8 TU Dolastatin-10 376128 9.53 0.42 4 47.0 T1 "Camptothecin,10-OH" 107124 7.51 0.56 7 35.7 ALK A7 C1 119875 Cisplatin TU Halichondrin B 609395 8.93 0.48 4 47.8 T1 "Camptothecin,11-formyl (RS)" 606172 5.69 0.69 3 50.3 TU Maytansine 153858 8.23 0.33 5 52.2 T1 "Camptothecin,11-HOMe (RS)" 606173 5.43 0.60 2 46.5 TU Trityl-cysteine 83265 6.01 0.51 15 42.7 T1 "Camptothecin,20-ester (S)" 606497 6.51 0.75 4 50.5 ALK A7 C2 132313 Dianhydrogalactitol bis-epoxide TU Vinblastine-sulfate 49842 9.04 1.00 134 39.0 T1 "Camptothecin,20-ester (S)" 606985 7.42 0.79 2 51.5 TU Vincristine-sulfate 67574 6.82 0.65 60 37.8 T1 "Camptothecin,20-ester (S)" 610456 6.84 0.74 4 51.5 TU Taxol (Paclitaxel) 125973 7.35 0.59 14 55.2 T1 "Camptothecin,20-ester (S)" 618939 7.19 0.75 3 51.7 ALK A7 C2 135758 Piperazinedione probably N-mustard-like with C2 TU Taxol analog 600222 5.65 0.68 2 54.5 T2 Amonafide 308847 5.49 0.21 16 39.9 TU Taxol analog 656178 5.66 0.75 2 49.5 T2 Amsacrine 249992 6.32 0.70 135 42.5 T2 T2 141540 Etoposide TU Taxol analog 658831 5.43 0.83 2 50.0 T2 Anthrapyrazole-derivative 355644 6.68 0.68 9 48.2 TU Taxol analog 661746 6.86 0.60 2 51.5 T2 Bisantrene 337766 6.76 0.67 11 39.4 TU Taxol analog 664402 6.85 0.71 2 49.5 T2 Daunorubicin 82151 7.10 0.58 78 45.8 TU Taxol analog 664404 7.80 1.11 2 51.0 T2 Deoxydoxorubicin 267469 7.34 0.55 7 49.3 TU Taxol analog 666608 7.00 0.72 2 54.0 T2 Doxorubicin 123127 6.84 0.56 1171 54.8 TU Taxol analog 671867 7.59 0.93 2 52.5 T2 Etoposide 141540 5.36 0.65 43 37.6 TU Taxol analog 671870 6.11 0.59 2 55.5 T2 Menogaril 269148 6.07 0.62 15 43.6 T2 T2 Db In 164011 Zorubicin (Rubidazone) TU Taxol analog 673187 6.43 0.85 2 56.0 T2 Mitoxantrone 301739 7.19 0.71 13 40.1 ALK A7 C2 167780 Asaley peptide mustard TU Taxol analog 673188 7.30 0.97 2 54.5 T2 Oxanthrazole (piroxantrone) 349174 5.83 0.44 14 43.0 T1 T1 176323 "CPT,9-MeO" active P90 Geldanamycin 330500 6.26 0.60 12 42.4 T2 Teniposide 122819 6.35 0.65 13 42.6 ALK A7 C2 Re 182986 Diaziridinylbenzoquinone Uk 3-Hydropicolinaldehyde-thiosemicarbazone 95678 5.79 0.40 15 43.3 T2 Zorubicin (Rubidazone) 164011 6.59 0.49 16 40.6 Uk 5-Hydroxypicolinaldehyde-thiosemicarbazone 107392 5.01 0.45 14 43.0 Pi L-Asparaginase 109229 -0.35 0.64 104 40.6 Uk Inosine-glycodialdehyde 118994 3.54 0.33 16 38.4 "*Alkylating agents: A2, A7 = alkylating at N-2, N-7 position of guanine, respectively; A6 = alkylating at O-6 position of guanine; T1 = topoisomerase I inhibitor; T2 = topoisomerase II inhibitor;" Db = DNA binder; Di = DNA incorporation; Df: antifols; Dr = ribonucleotide reductase inhibitor; Ds = DNA synthesis inhibitor; Rs = RNA synthesis inhibitor; Tu = tubulin-active antimitotic agents; Pi = protein synthesis inhibitor; P90 = hsp90 binder; Uk = unknown